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2015 ; 87
(ä): 81-9
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Bioconjugates for targeted delivery of therapeutic oligonucleotides
#MMPMID25689735
Ming X
; Laing B
Adv Drug Deliv Rev
2015[Jun]; 87
(ä): 81-9
PMID25689735
show ga
Bioconjugates have been used to deliver therapeutic oligonucleotides to their
pharmacological targets in diseased cells. Molecular-scale conjugates can be
prepared by directly linking targeting ligands with oligonucleotides and the
resultant conjugates can selectively bind to cell surface receptors in target
cells in diseased tissues. Besides targeted delivery, additional functionality
can be incorporated in the conjugates by utilization of carrier molecules, and
these larger conjugates are called carrier-associated conjugates. Both molecular
and carrier-associated conjugates have achieved initial successes in clinical
trials for treating liver diseases; therefore, currently the greater challenge is
to deliver oligonucleotides to extrahepatic tissues such as tumors. This review
will provide an update on the application of oligonucleotide conjugates for
targeted delivery during the last decade. By identifying key elements for
successful delivery, it is suggested that oligonucleotide conjugates with
intermediate size, cell targeting ability, and endosomal release functionality
are superior systems to advance oligonucleotides to achieve their full
therapeutic potentials.